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Hydrochlorothiazide crystal and candesartan cilexetil hydrochlorothiazide medicinal combination thereof

A technology of candesartan cilexetil and hydrochlorothiazide, which is applied in the field of medicine and can solve problems such as poor bioavailability, slow dissolution of hydrochlorothiazide, and unsatisfactory curative effect of pharmaceutical preparations

Active Publication Date: 2013-08-07
HAINAN JINRUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Patent application CN101659643A discloses a crystal form of hydrochlorothiazide and its use. Aiming at the problems of slow dissolution and poor bioavailability of hydrochlorothiazide commonly found in the prior art, a new hydrochlorothiazide crystal form III (such as figure 2 shown), the results show that the dissolution rate of preparations made of hydrochlorothiazide crystal form III or the composition of hydrochlorothiazide III and other types of antihypertensive drugs can reach a level similar to that of similar foreign products, and solve the problem of hydrochlorothiazide dissolution to a certain extent. slow speed problem
However, the stability of the preparation has not been significantly improved, and the curative effect of the pharmaceutical preparation is not ideal. In view of this, the present invention is proposed

Method used

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  • Hydrochlorothiazide crystal and candesartan cilexetil hydrochlorothiazide medicinal combination thereof
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  • Hydrochlorothiazide crystal and candesartan cilexetil hydrochlorothiazide medicinal combination thereof

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Embodiment 1

[0084] The preparation of embodiment 1 hydrochlorothiazide crystal

[0085] (1) 1kg hydrochlorothiazide is dissolved in acetone to obtain acetone solution whose concentration is 0.1g / ml hydrochlorothiazide;

[0086] (2) Add distilled water dropwise to the acetone solution under stirring at 160r / min until the solution becomes turbid;

[0087] (3) under the ultrasonic field that power is 0.5KW, flow the organic mixed solution of ethanol and ether in the solution gained in step 2, continue the stirring of 25r / min; Wherein the volume ratio of ethanol and ether in the organic mixed solution is 5: 6, The volume ratio of described mixed solution and acetone is 1: 1;

[0088] (4) Continue ultrasonication for 2 minutes, let stand, grow crystals at 16° C. for 2 hours, filter, wash the filter cake with ether, and vacuum-dry to obtain hydrochlorothiazide crystals.

[0089] Such as figure 1 As shown, the characteristic peaks in the X-ray powder diffraction pattern obtained by measuring...

Embodiment 2

[0090] The preparation of embodiment 2 hydrochlorothiazide crystals

[0091] (1) 1kg hydrochlorothiazide is dissolved in acetone to obtain acetone solution whose concentration is 0.2g / ml hydrochlorothiazide;

[0092] (2) Add distilled water dropwise to the acetone solution under stirring at 120r / min until the solution becomes turbid;

[0093] (3) under the ultrasonic field that power is 0.4KW, flow the organic mixed solution of ethanol and ether in the solution gained in step 2, continue the stirring of 20r / min; Wherein the volume ratio of ethanol and ether in the organic mixed solution is 2: 3, The volume ratio of described mixed solution and acetone is 4: 5;

[0094] (4) Continue ultrasonication for 2 minutes, let stand, grow crystals at 12° C. for 1.5 hours, filter, wash the filter cake with ether, and vacuum-dry to obtain hydrochlorothiazide crystals.

[0095] Such as figure 1 As shown, the characteristic peaks in the X-ray powder diffraction pattern obtained by measur...

Embodiment 3

[0096] The preparation of embodiment 3 hydrochlorothiazide crystals

[0097] (1) 1kg hydrochlorothiazide is dissolved in acetone to obtain a solution of acetone with a concentration of 0.08g / ml hydrochlorothiazide;

[0098] (2) Add distilled water dropwise to the acetone solution under stirring at 180r / min until the solution becomes turbid;

[0099] (3) under the ultrasonic field that power is 0.6KW, flow the organic mixed solution of ethanol and ether in the solution gained in step 2, continue the stirring of 30r / min; Wherein the volume ratio of ethanol and ether in the organic mixed solution is 7: 6, The volume ratio of described mixed solution and acetone is 8:5;

[0100] (4) Continue ultrasonication for 3 minutes, let stand, grow crystals at 18° C. for 2.5 hours, filter, wash the filter cake with ether, and vacuum-dry to obtain hydrochlorothiazide crystals.

[0101] Such as figure 1 As shown, the characteristic peaks in the X-ray powder diffraction pattern obtained by ...

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Abstract

The invention discloses a hydrochlorothiazide crystal and a candesartan cilexetil hydrochlorothiazide medicinal combination thereof. The characteristic peaks of the hydrochlorothiazide crystal in an X-ray powder diffraction pattern, which are measured and obtained by using a Cu-K[alpha] ray, are displayed when 2[theta] is 4.1 degrees, 8.2 degrees, 9.8 degrees, 12.1 degrees, 15.1 degrees, 16.7 degrees, 19.3 degrees, 20.0 degrees, 22.1 degrees, 23.3 degrees and 26.8 degrees. The combination comprises 4-20 parts of candesartan cilexetil, 10-15 parts of the hydrochlorothiazide crystal, 10-50 parts of pregelatinized starch, 15-35 parts of microcrystalline cellulose PH102, 10-45 parts of crosslinked polyvinylpyrrolidone and 0.5-1 part of magnesium stearate. The medicinal combination has a reasonable prescription, stable and reliable quality, and better disintegration time limit and dissolution rate; a direct powder tabletting process is adopted; the process is simple; the production period is short; the production cost is low; and the industrialized production is facilitated.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a hydrochlorothiazide crystal and a candesartan cilexetil hydrochlorothiazide pharmaceutical composition. Background technique [0002] Hypertension is the most common cardiovascular disease and a major public health problem worldwide. In 1991, my country conducted a sample survey of 940,000 people over the age of 15. Statistics show that the prevalence of hypertension in my country has reached 11.26%, which is 25% higher than that in the 10 years from 1979 to 1990. There are more than 130 million hypertensive patients in my country. . Moreover, this upward momentum continues. Statistics also show that the treatment rate of hypertension is 17.4% in urban areas and 5.4% in rural areas; the control rate (systolic blood pressure<140mmHg and diastolic blood pressure<90mmHg after treatment) is only 2.9%. From the above statistics, it can be seen that the prevalenc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D285/28A61K31/549A61K31/4184A61K9/20A61K9/48A61P9/12
Inventor 钟正明罗韬王小树马鹰军
Owner HAINAN JINRUI PHARMA CO LTD
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